Johnson & Johnson

Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.

Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.

Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It has been used for monotherapy of Parkinson′s disease in the early phase; combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson′s disease and adjunctive therapy of prolactin-producing pituitary gland tumors (microprolactinomas).

Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage

JNJ-10198409 is a potent ATP-competitive inhibitor of Platelet-Derived Growth Factor receptor tyrosine kinase (PDGF-RTK) with both antiangiogenicand a directtumor cell antiproliferative activity. It is selective for PDGF-β kinase with IC50 values of 4.2 nM for PDGF-β and 45 nM for PDGF-α kinase.

JNJ-1661010 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with >100-fold preferentially selective for FAAH-1 over FAAH-2. FAAH in an integral membrane enzyme within the amidase-signature family. It catalyzes the hydrolysis of several endogenous biologically active lipids and involves in a variety of physiological and pathological processes, including synaptic regulation, regulation of sleep and feeding, locomotor activity, pain and inflammation.

MBX-102 has a potent transrepression effect on PPARγ. It is an oral glucose-reducing agent and also has insulin-sensitizing properties. It is useful as treatment for type 2 diabetes. MBX-102 also lowers triglycerides in a PPARα-independent manner.MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ. MBX-102 is converted to the active form, MBX-102 acid, in vivo.

Kainate GluR5 receptor antagonist; anticonvulsant.Topiramate is a derivative of suphamate fructopyranose that inhibits the release of mesocorticolimbic dopamine. It facilitates GABA activity and inhibits glutamate function to alleviate the rewarding effects of alcohol. It modulates the trigeminovascular signaling that is effective in migraine prevention. Topiramate is structurally similar to fructose- 1,6-diphosphate and has the ability to inhibit the enzyme fructose 1,6-bisphosphatase, thereby preventing gluconeogenesis. It is found to inhibit the AMPA/kainate receptor-mediated signaling pathway in cultured neurons.